Pharmacology Mnemonics - Flash Cards

Name: G-CSF (Filgrastim)

Class: Immunostimulant

Mechanism: Promotes growth & differentiation of granulocyte precursors.

Absorption:

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Excretion, t½:

Toxicity/S.E.s: Bone pain, fever, anti-CSF antibodies.

Utility: Restore hematopoiesis (FDA-approved to treat neutropenia), augment host defenses, esp. after cancer therapy.

Name: Antilymphocyte Globulin (ALG)

Class: Immunosuppressant

Mechanism: Polyclonal antibody to human lymphocytes (not selective to CD3) ® destruction and inactivation of lymphocytes.

Absorption:

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Excretion, t½:

Toxicity/S.E.s: Chills, fever, thrombocytopenia, erythema, pruritis, hypersensitivity rxns, anti-ALG antibody production (\ only given for 1-2 weeks).

Utility: Prevent or reverse acute allograft rejection.

Special Features:

Name: Cyclophosphamide (Cytoxan)

Class: Immunosuppressant (Alkylating Agent) (Cancer Chemotherapeutic Agent)

Mechanism: Activated via hepatic P450 Metabolismolism ® phosphoramide mustard. Phosphoramide mustard alkylates DNA ® cytotoxicity to dividing cells.

Absorption: Oral

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Excretion, t½:

Toxicity/S.E.s: Bone marrow depression (esp. leukocytosis), hemorrhagic cystitis (may ® bladder fibrosis), n/v/d, alopecia, amenorrhea, testicular atrophy, sterility. Possible secondary malignancies years later.

Utility: Cancer chemotherapy, nephrotic syndrome, intractable rheumatoid arthritis.

Special Features: Therapeutic effect independent of level of P450 activity.

Name: Azathioprine (Imuran)

Class: Immunosuppressant (AntiMetabolismolite)

Mechanism: Converted to 6-mercaptopurine (thiol analog of hypoxanthine) ® inhib. of purine synth. ® cytotoxicity to dividing cells ® ¯ lymphocyte proliferation ® inhib. of cellular and humoral immunity.

Absorption:

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Excretion, t½:

Toxicity/S.E.s: Bone marrow depression (main toxicity), n/v/d, hepatotoxicity.

Utility: Primarily used in maintenance of remission in acute lymphoblastic leukemia.

Special Features:

Name: Methylprednisone

Class: Corticosteroid (Immunosuppressant)

Mechanism: Inhib. of IL-1 & TNF synth/release from Mfs ® ¯ activation of T cells and Mfs, ¯ PMN fxn, ¯ T cell-dependent Ab production, ¯ complement activity, ¯ activity & release of kinins.

Absorption: Parenteral

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Excretion, t½:

Toxicity/S.E.s: Suppressed pituitary adrenal fxn, hypertension, weight gain, peptic ulcer, GI bleeding, euphoric personality changes, cataracts, hyperglycemia.

Utility: Immunosuppression. Primarily employed to induce remission in patients w/acute lymphocytic leukemia, and in treatment of lymphomas.

Special Features:

Name: Prednisone

Class: Corticosteroid (Immunosuppressant)

Mechanism: Inhib. of IL-1 & TNF synth/release from Mfs ® ¯ activation of T cells and Mfs, ¯ PMN fxn, ¯ T cell-dependent Ab production, ¯ complement activity, ¯ activity & release of kinins.

Absorption: Oral

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Excretion, t½:

Toxicity/S.E.s: Suppressed pituitary adrenal fxn, hypertension, weight gain, peptic ulcer, GI bleeding, euphoric personality changes, cataracts, hyperglycemia.

Utility: Immunosuppression. Primarily employed to induce remission in patients w/acute lymphocytic leukemia, and for treatment of lymphomas. Treat hypercalcemia due to vit. D intox., sarcoidosis, or specific cancers (e.g., lymphoproliferative) (30-60 mg/d).

Special Features:

Name: OKT3 (Muromonab-CD3)

Class: Immunosuppressant

Mechanism: Opsonizes T cells, modulates CD3 antigen recognition complex on T cells, blocks CTL killer function.

Absorption: IV

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Excretion, t½:

Toxicity/S.E.s: Chills, fever, thrombocytopenia, erythema, pruritis, hypersensitivity rxns, anti-OKT3 antibody production (\ only given for 1-2 weeks).

Utility: Prevent or reverse acute allograft rejection.

Special Features: Murine monoclonal antibody against CD3 on T cells.

Name: Cyclosporine (Sandimmune)

Class: Immunosuppressant

Mechanism: Binds to calmodulin and a cytoplasmic cytophilin ® selective inhib. of transcription of IL-2 gene ® inhib. of IL-2 prod. & release from T4 cells, inhib. of proliferation of T8 cells, block of T4 activation of B cells.

Absorption: Oral ® highly variable and incomplete absorption.

Dist.: Large Vd. Binds in tissues. 60-70% contained in RBCs.

Metabolism.: Extensive hepatic Metabolism involving cyt. P450 enzymes. 17 Metabolismolites known. Drug levels monitored by RIA or HPLC.

Excretion, t½: Biliary excretion, minor renal excretion.

Toxicity/S.E.s: Nephrotoxicity (main toxicity), hepatotoxicity, hirsutism, gingival hyperplasia, neurotoxicity, altered coagulability. But little (if any) bone marrow suppression. Drug interactions—rifampin & phenobarbital ® induction of hepatic Metabolism. Erythromycin ® inhib. of hepatic Metabolism. Ketoconazole & amphotericin ® ¯ clearance.

Utility: Prolong organ transplants (1° use). Suppress cell-med. diseases. Possible benefit w/early treatment of IDDM.

Special Features: